A83-01, TGF-β Inhibitor


Catalog No. size PriceQuantity
M60021-2S 2 mg solid $79
M60021-25S 25mg solid $320

Description

Product Information
Chemical Name: 3-(6-methylpyridin-2-yl)-N-phenyl-4-(quinolin-4-yl)-1H-pyrazole-1-carbothioamide
Molecular Weight: 421.52
Formula: C25H19N5S
Purity: ≥98%
CAS#: 909910-43-6
Solubility: DMSO up to 100 mM
Storage: Powder: 4oC 1 year DMSO: 4oC 3 month -20oC 1 year



Biological Activity:

A83-01 is a potent and selective T TGF-β pathway inhibitor. It inhibits ALK5 (IC50~12 nM), ALK4 (IC50~45 nM) and ALK7 (IC50~7.5nM). It only has weak inhibitory activity on ALK1, 2, 3, and 6. It blocks phosphorylation of Smad2 and inhibits  TGF-β-induced epithelial-to-mesenchymal transition. A83-01 has been used to enhance iPSC reprogramming, induce neural differentiation of human pluripotent stem cells, and promote naive state of pluripotent stem cells.


How to Use:

In vitro: A83-01 is typically used at 10 µM as final concentration in cell culture.

In vivo: A83-01 was orally dosed to mice at 100-200 mg/kg once per day or intraperitoneally dosed to mice at 10-100 mg/kg once per day.


Reference:

  1. Tojo M, et al. The ALK-5 inhibitor A-83-01 inhibits smad signaling and epithelial-to-mesenchymal transition by transforming growth factor-beta. (2005) Cancer Science 96 (11), 791-800.
  2. i W, et al. Generation of rat and human induced pluripotent stem cells by combining genetic reprogramming and chemical inhibitors. (2009) Cell Stem Cell 4(1), 16-19.
  3. Yuan X, et al. Combined Chemical Treatment Enables Oct4-Induced Reprogramming from Mouse Embryonic Fibroblasts. (2011) Stem Cells 29(3), 549¨C553.
  4. Klincumhom N, et al. Selective TGF-β1/ALK inhibitor improves neuronal differentiation of mouse embryonic stem cells. (2014) Neurosci Lett. 578:1-6.

Products are for research use only. Not for human use.

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